Applications
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In SET2 and Ba/F3 cells engineered to express JAK2V617F, BMS-911543 exhibited a dose-dependent anti-proliferative effect with IC50 values of 60 and 70 nM, respectively. In human platelets, BMS-911543 inhibited TPO-stimulated pSTAT5 in a dose-dependent manner. In primary hematopoetic progenitor cells isolated from MPN patients that expressed JAK2V617F, JAK2EXON12 or MPLW515L mutations, BMS-911543 inhibited EPO-mediated burst forming unit-erythroid (BFU-E) colony growth with IC50 ranging from <0.150 to ~0.9 μM.
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References:
[1] Purandare AV, McDevitt TM, Wan H, You D, Penhallow B, Han X, Vuppugalla R, Zhang Y, Ruepp SU, Trainor GL, Lombardo L, Pedicord D, Gottardis MM, Ross-Macdonald P, de Silva H, Hosbach J, Emanuel SL, Blat Y, Fitzpatrick E, Taylor TL, McIntyre KW, Michaud E, Mulligan C, Lee FY, Woolfson A, Lasho TL, Pardanani A, Tefferi A, Lorenzi MV. Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2. Leukemia. 2012 Feb;26(2):280-8.
[2]. Wan H1, Schroeder GM1, Hart AC1, et al. Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms. ACS Med Chem Lett. 2015 Jul 12;6(8):850-5.
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